Lopinavir

SKU: orb1307985

Description

Lopinavir (ABT-378) is a peptidomimetic inhibitor of HIV-1 protease that maintains efficacy against the Val82 mutant variant and exhibits reduced serum protein binding compared to ritonavir. It is widely used in antiviral research for in vitro enzyme assays and in vivo studies of HIV infection and resistance mechanisms.

Research Area

Infectious Disease & Virology, Pharmacology & Drug Discovery, Protein Biochemistry

Key Properties

• CAS Number: 192725-17-0
• MW: 628.8008
• Purity: 99.62% (May vary between batches)
• Formula: C₃₇H₄₈N₄O₅
• SMILES: CC(C)[C@H](N1CCCNC1=O)C(=O)N[C@H](C[C@H](O)[C@H](CC1=CC=CC=C1)NC(=O)COC1=C(C)C=CC=C1C)CC1=CC=CC=C1
• Target: HIV Protease,SARS-CoV
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (6.36 mM);DMSO:247.5 mg/mL (393.61 mM);Ethanol:116 mg/mL (184.48 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  HIV protease:1.3 pM(Ki)
• In Vivo:
  Lopinavir is an effective inhibitor of Rh123, with an IC50 value of 1.7 mM for Caco-2 cell monolayers. It binds to mutant HIV proteases (V82A, V82T, and V82F) with Ki values of 4.9, 3.7, and 3.6 pM, respectively. At a concentration of 0.5 nM, Lopinavir inhibits the activity of wild-type HIV protease by 93%. It also inhibits HIV protease activity in MT4 cells both in the presence and absence of 50% HS, with EC50 values of 102 nM and 17 nM, respectively. In liver microsomes, Lopinavir is converted to primary metabolites M-3 and M-4, a process that is NADPH-dependent. After treating LS 180V cells with Lopinavir for 72 hours, there is a reduction in intracellular Rh123 content and induction of P-glycoprotein immunoreactive protein and mRNA levels. Lopinavir exhibits an IC50 of 9.4 nM against subtype C clone C6. When acting on human liver microsomes, Lopinavir shows an IC50 of 7.3 mM against CYP3A and exerts weak inhibition on human CYP1A2, 2B6, 2C9, 2C19, and 2D6.
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• In Vitro:
  Administering Lopinavir (10 mg/kg, p.o.) to rats resulted in a maximum concentration (Cmax) of 0.8 μg/mL, with the drug's bioavailability being 25%.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

coadministration, ABT378, ABT-378, ABT 378, infection, inhibit, mutant, Lopinavir, Inhibitor, Human immunodeficiency virus, HIV protease, HIVProtease, HIV Protease, HIV, SARS-CoV, SARS coronavirus, SARSCoV, replication, wild-type

Compound Identifiers

PubChem CID

92727